Protein Lysine Methyltransferase Inhibitor, UNC0321-Calbiochem

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一般描述

A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC₅₀= 6 nM and 9 nM in two biochemical assays for CLOT and ECSD, respectively, and K_i= 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX01294 (Cat. No. 382190)). It inhibits GLP with reduced potency (15 nM) and is found to be inactive (IC₅₀>40 ?M) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3, as well as JMJD2E (>1000-fold selectivity) in ECSD enzymatic assays. It also inhibits H3K9me2 accumulation (IC₅₀= 11,000 nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC₅₀= 500 nM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable quinazoline analog that potently and selectively inhibits PKMT G9a with IC₅₀s equal to 6 ?M and 9 ?M in two biochemical assays (CLOT and ECSD respectively), and a Morrison K_iof 63 pM, which is about 250-fold more potent compared with a close analog BIX01294 (Cat. No. 382190). Also inhibited GLP with reduced potency (15 ?M in an ECSD enzymatic assay). It was found to be inactive (IC₅₀>40 ?M) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3 in the ECSD assays as well as JMJD2E with >1000-fold selectivity.

包装

5 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Liu, F., et al. 2010.J. Med. Chem.53,5844.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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